JP6633246B2 - ヒトｐｄｅ１阻害薬として有用なトリアゾロピラジノン誘導体 - Google Patents
ヒトｐｄｅ１阻害薬として有用なトリアゾロピラジノン誘導体 Download PDFInfo
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- JP6633246B2 JP6633246B2 JP2019510969A JP2019510969A JP6633246B2 JP 6633246 B2 JP6633246 B2 JP 6633246B2 JP 2019510969 A JP2019510969 A JP 2019510969A JP 2019510969 A JP2019510969 A JP 2019510969A JP 6633246 B2 JP6633246 B2 JP 6633246B2
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- 102000050549 human PDE7B Human genes 0.000 description 1
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 150000002466 imines Chemical class 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 230000037041 intracellular level Effects 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- MGFYIUFZLHCRTH-UHFFFAOYSA-N nitrilotriacetic acid Chemical compound OC(=O)CN(CC(O)=O)CC(O)=O MGFYIUFZLHCRTH-UHFFFAOYSA-N 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 238000007339 nucleophilic aromatic substitution reaction Methods 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 238000007243 oxidative cyclization reaction Methods 0.000 description 1
- 229910052763 palladium Inorganic materials 0.000 description 1
- 101150037969 pde-6 gene Proteins 0.000 description 1
- 230000037081 physical activity Effects 0.000 description 1
- 239000003880 polar aprotic solvent Substances 0.000 description 1
- 239000002798 polar solvent Substances 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 125000001567 quinoxalinyl group Chemical class N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000006722 reduction reaction Methods 0.000 description 1
- 238000006268 reductive amination reaction Methods 0.000 description 1
- 230000008327 renal blood flow Effects 0.000 description 1
- 201000002793 renal fibrosis Diseases 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 238000001542 size-exclusion chromatography Methods 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 229910052723 transition metal Inorganic materials 0.000 description 1
- 150000003624 transition metals Chemical class 0.000 description 1
- 230000014616 translation Effects 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- JABYJIQOLGWMQW-UHFFFAOYSA-N undec-4-ene Chemical compound CCCCCCC=CCCC JABYJIQOLGWMQW-UHFFFAOYSA-N 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- 230000037221 weight management Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Urology & Nephrology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662379372P | 2016-08-25 | 2016-08-25 | |
| US62/379,372 | 2016-08-25 | ||
| PCT/US2017/047479 WO2018039051A1 (en) | 2016-08-25 | 2017-08-18 | Triazolopyrazinone derivative useful as a human pde1 inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019526567A JP2019526567A (ja) | 2019-09-19 |
| JP6633246B2 true JP6633246B2 (ja) | 2020-01-22 |
Family
ID=59762063
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019510969A Active JP6633246B2 (ja) | 2016-08-25 | 2017-08-18 | ヒトｐｄｅ１阻害薬として有用なトリアゾロピラジノン誘導体 |
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| EP (1) | EP3504208B1 (lt) |
| JP (1) | JP6633246B2 (lt) |
| KR (1) | KR20190028544A (lt) |
| CN (1) | CN109641902B (lt) |
| AR (1) | AR109328A1 (lt) |
| AU (1) | AU2017317111A1 (lt) |
| BR (1) | BR112019000988A2 (lt) |
| CA (1) | CA3034828A1 (lt) |
| CL (1) | CL2019000487A1 (lt) |
| CO (1) | CO2019001644A2 (lt) |
| CR (1) | CR20190078A (lt) |
| CY (1) | CY1123406T1 (lt) |
| DK (1) | DK3504208T3 (lt) |
| DO (1) | DOP2019000021A (lt) |
| EA (1) | EA201990313A1 (lt) |
| EC (1) | ECSP19013196A (lt) |
| ES (1) | ES2800433T3 (lt) |
| HR (1) | HRP20201187T1 (lt) |
| HU (1) | HUE050419T2 (lt) |
| JO (1) | JOP20170164A1 (lt) |
| LT (1) | LT3504208T (lt) |
| MA (1) | MA46039B1 (lt) |
| MD (1) | MD3504208T2 (lt) |
| ME (1) | ME03791B (lt) |
| MX (1) | MX2019002065A (lt) |
| PE (1) | PE20190452A1 (lt) |
| PH (1) | PH12019500370A1 (lt) |
| PL (1) | PL3504208T3 (lt) |
| PT (1) | PT3504208T (lt) |
| RS (1) | RS60442B1 (lt) |
| SG (1) | SG11201901311WA (lt) |
| SI (1) | SI3504208T1 (lt) |
| SV (1) | SV2019005838A (lt) |
| TN (1) | TN2019000038A1 (lt) |
| TW (1) | TWI651323B (lt) |
| WO (1) | WO2018039051A1 (lt) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020529413A (ja) * | 2017-08-02 | 2020-10-08 | イーライ リリー アンド カンパニー | ［１，２，４］トリアゾロ［４，３−ａ］ピラジン−６（５ｈ）−オン誘導体 |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201920188A (zh) | 2017-08-10 | 2019-06-01 | 美商美國禮來大藥廠 | [1,2,4]三唑衍生物 |
| US11453673B2 (en) | 2018-02-06 | 2022-09-27 | Eli Lilly And Company | Substituted [1,2,4]triazolo[4,3-a]pyrazines as phosphodiesterase inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4354027A (en) | 1980-05-19 | 1982-10-12 | Usv Pharmaceutical Corporation | Triazoloquinoxalin-4-ones |
| EP2103613B1 (en) | 2006-12-13 | 2016-02-17 | ASKA Pharmaceutical Co., Ltd. | Quinoxaline derivative |
| WO2008103357A1 (en) | 2007-02-21 | 2008-08-28 | E. I. Du Pont De Nemours And Company | Fungicidal tricyclic 1,2,4-triazoles |
| PT2615096T (pt) | 2010-09-07 | 2019-10-15 | Astellas Pharma Inc | Composto de quinoxalina |
| US9499562B2 (en) | 2012-06-18 | 2016-11-22 | Dart Neuroscience (Cayman) Ltd. | Substituted thiophene- and furan-fused azolopyrimidine-5-(6H)-one compounds |
| WO2016022825A1 (en) * | 2014-08-07 | 2016-02-11 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US20160083400A1 (en) * | 2014-09-18 | 2016-03-24 | Sunovion Pharmaceuticals Inc. | Tricyclic guanidine derivative |
| TW201629064A (zh) * | 2014-10-10 | 2016-08-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之三唑並吡酮 |
| TWI609870B (zh) | 2016-02-12 | 2018-01-01 | 美國禮來大藥廠 | Pde1抑制劑 |
-
2016
- 2016-08-25 JO JOP/2017/0164A patent/JOP20170164A1/ar unknown
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2017
- 2017-08-11 AR ARP170102252A patent/AR109328A1/es unknown
- 2017-08-11 TW TW106127199A patent/TWI651323B/zh not_active IP Right Cessation
- 2017-08-18 KR KR1020197005013A patent/KR20190028544A/ko not_active Application Discontinuation
- 2017-08-18 PE PE2019000371A patent/PE20190452A1/es unknown
- 2017-08-18 MD MDE20190732T patent/MD3504208T2/ro unknown
- 2017-08-18 EP EP17761381.7A patent/EP3504208B1/en active Active
- 2017-08-18 WO PCT/US2017/047479 patent/WO2018039051A1/en unknown
- 2017-08-18 SG SG11201901311WA patent/SG11201901311WA/en unknown
- 2017-08-18 SI SI201730305T patent/SI3504208T1/sl unknown
- 2017-08-18 MA MA46039A patent/MA46039B1/fr unknown
- 2017-08-18 CA CA3034828A patent/CA3034828A1/en not_active Abandoned
- 2017-08-18 PT PT177613817T patent/PT3504208T/pt unknown
- 2017-08-18 EA EA201990313A patent/EA201990313A1/ru unknown
- 2017-08-18 PL PL17761381T patent/PL3504208T3/pl unknown
- 2017-08-18 BR BR112019000988-4A patent/BR112019000988A2/pt not_active IP Right Cessation
- 2017-08-18 ES ES17761381T patent/ES2800433T3/es active Active
- 2017-08-18 ME MEP-2020-144A patent/ME03791B/me unknown
- 2017-08-18 LT LTEP17761381.7T patent/LT3504208T/lt unknown
- 2017-08-18 HU HUE17761381A patent/HUE050419T2/hu unknown
- 2017-08-18 AU AU2017317111A patent/AU2017317111A1/en not_active Abandoned
- 2017-08-18 TN TNP/2019/000038A patent/TN2019000038A1/en unknown
- 2017-08-18 DK DK17761381.7T patent/DK3504208T3/da active
- 2017-08-18 RS RS20200738A patent/RS60442B1/sr unknown
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- 2017-08-18 MX MX2019002065A patent/MX2019002065A/es unknown
- 2017-08-18 US US15/680,250 patent/US10138244B2/en active Active
- 2017-08-18 JP JP2019510969A patent/JP6633246B2/ja active Active
- 2017-08-18 CN CN201780050004.2A patent/CN109641902B/zh active Active
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2019
- 2019-01-30 DO DO2019000021A patent/DOP2019000021A/es unknown
- 2019-02-19 SV SV2019005838A patent/SV2019005838A/es unknown
- 2019-02-21 PH PH12019500370A patent/PH12019500370A1/en unknown
- 2019-02-22 CO CONC2019/0001644A patent/CO2019001644A2/es unknown
- 2019-02-22 CL CL2019000487A patent/CL2019000487A1/es unknown
- 2019-02-22 EC ECSENADI201913196A patent/ECSP19013196A/es unknown
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2020
- 2020-07-29 HR HRP20201187TT patent/HRP20201187T1/hr unknown
- 2020-08-14 CY CY20201100760T patent/CY1123406T1/el unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020529413A (ja) * | 2017-08-02 | 2020-10-08 | イーライ リリー アンド カンパニー | ［１，２，４］トリアゾロ［４，３−ａ］ピラジン−６（５ｈ）−オン誘導体 |
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